A CFTR potentiator; increases the forskolin-induced CFTR-mediated epithelial current in cells expressing the G551D missense mutation by ~4-fold (EC50 = 100 nM); increases chloride secretion in cultured human cystic fibrosis bronchial epithelial cells carrying the G551D mutation on one allele and the common ΔF508 processing mutation on the other allele; binds CFTR directly and leads to CFTR channel opening via an ATP-independent mechanism

Ivacaftor – 1 mg

Brand:
Cayman
CAS:
873054-44-5
Storage:
-20
UN-No:
Non-Hazardous - /

Ivacaftor is an orally bioavailable potentiator of the cystic fibrosis transmembrane conductance regulator (CFTR) that improves chloride transport.{25614} It increases the forskolin-induced CFTR-mediated epithelial current in cells expressing the G551D missense mutation associated with severe cystic fibrosis by approximately 4-fold (EC50 = 100 nM) but has no effect on current in the absence of forskolin.{25614} Ivacaftor increases chloride secretion in cultured human cystic fibrosis bronchial epithelial cells carrying the G551D mutation on one allele and the common ΔF508 processing mutation on the other allele.{25614} It binds CFTR directly and leads to CFTR channel opening via an ATP-independent mechanism.{25613} Formulations containing ivacaftor have been used in the treatment of cystic fibrosis in patients carrying one or more mutations in the CFTR gene.  

 

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Description

A CFTR potentiator; increases the forskolin-induced CFTR-mediated epithelial current in cells expressing the G551D missense mutation by ~4-fold (EC50 = 100 nM); increases chloride secretion in cultured human cystic fibrosis bronchial epithelial cells carrying the G551D mutation on one allele and the common ΔF508 processing mutation on the other allele; binds CFTR directly and leads to CFTR channel opening via an ATP-independent mechanism

Formal name: N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxo-3-quinolinecarboxamide

Synonyms:  VX 770

Molecular weight: 392.5

CAS: 873054-44-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Activators||Research Area|Immunology & Inflammation|Pulmonary Diseases|Cystic Fibrosis

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